6-Benzothiazolyl Ureas, Thioureas and Guanidines are Potent Inhibitors of ABAD/17 beta-HSD10 and Potential Drugs for Alzheimer's Disease Treatment: Design, Synthesis and in vitro Evaluation

摘要

Background: The mitochondrial enzyme amyloid beta-binding alcohol dehydrogenase (ABAD) also known as 17 beta-hydroxysteroid dehydrogenase type 10 (17 beta-HSD10) has been connected with the pathogenesis of Alzheimer's disease (AD). ABAD/17 beta-HSD10 is a binding site for the amyloid-beta peptide (A beta) inside the mitochondrial matrix where it exacerbates A beta toxicity. Interaction between these two proteins triggers a series of events leading to mitochondrial dysfunction as seen in AD.